Influence of salivary washout on drug delivery to the oral cavity using coated microneedles: An in vitro evaluation

The objective of this study was to determine whether in buccal tissues, after insertion and removal of coated microneedles, the presence of saliva over the insertion site can lead to loss of the deposited drug, and if saliva can influence in vitro permeation of the drug across the tissue. Microneedles were coated with sulforhodamine (SRD), which was used as a model drug, and inserted in to porcine buccal mucosa in vitro. Fluorescence microscopy was used to study microneedle coating quality and the diffusion of SRD through the mucosa. Permeation experiments were conducted for simulated dynamic or static salivary flow by adding 100 μL/h or 100, 200 or 300 μL of phosphate buffered saline (PBS) in the donor compartment of the Franz diffusion cells, into which buccal tissue after insertion of SRD-coated microneedles was placed. Microscopy showed that microneedles were uniformly coated with SRD and that SRD was successfully delivered in to the mucosa. Some SRD remained in the tissue even after 24 h, despite presence of PBS on top of the coated microneedle insertion site. It was found that salivary washout can result in loss of drug that has been deposited in oral cavity mucosal tissues using coated microneedles, and presence of fluid over the coated microneedle insertion site can increase flux across the tissue. Thus, it is advisable to include salivary flow during in vitro studies related to the use of coated microneedles for drug delivery to the oral cavity in order to not obtain misleading results.

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